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Gastrin I is an endogenous, gastrointestinal peptide hormone that binds to cholecystokinin (CCK) receptors on human gastric leiomyosarcoma cells (IC50 = 0.9 nM) and in guinea pig gallbladder and pancreatic tissue (IC50s = 1.7 and 2.5 μM, respectively).1,2 It increases levels of cytosolic calcium in isolated rabbit stomach parietal cells (EC50 = 11 nM) and stimulates pepsinogen secretion by isolated human peptic cells (ED50 = 30 nM).3,4 Gastrin I increases histidine decarboxylase (HDC) activity ex vivo in fundic stomach mucosa homogenate and increases gastric acid secretion in vivo in rats when administered at a dose of 1 nmol/kg/h.5
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1. Characterization of cholecystokinin receptors on human gastric smooth muscle tumors. Am. J. Physiol. 247(4 Pt 1), G402-G410 (1984).
2. Cholecystokinin receptors on gallbladder muscle and pancreatic acinar cells: A comparative study. Am. J. Physiol. 255(4 Pt 1), G512-G521 (1988).
3. Cytosolic Ca2+ evaluation in rabbit parietal cells: A novel method to screen gastrin receptor antagonists. Eur. J. Pharmacol. 306(1-3), 325-333 (1996).
4. Effects of cholinergic, histaminergic, and peptidergic stimulation on pepsinogen secretion by isolated human peptic cells. Scand. J. Gastroenterol. 29(8), 678-683 (1994).
5. Effect of cholecystokinin receptor antagonists, MK-